Uses
NVP-BSK805 is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively[1].
in vivo
NVP-BSK805 (BSK 805; 150 mg/kg, p.o.) blocks STAT5 phosphorylation, splenomegaly, and leukemic cell spreading in a Ba/F3 JAK2V617F cell-driven mouse model[1].
NVP-BSK805 (50, 75, and 100 mg/kg, p.o.) also suppresses rhEpo-mediated polycythemia and splenomegaly in BALB/c mice[1].
IC 50
JAK2 JH1: 0.48 nM (IC
50); FL JAK2 V617F: 0.56 nM (IC
50); FL JAK2 wt: 0.58 nM (IC
50); TYK2 JH1: 10.76 nM (IC
50); JAK3 JH1: 18.68 nM (IC
50); JAK1 JH1: 31.63 nM (IC
50)
References
[1] Baffert F, et al. Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805. Mol Cancer Ther. 2010 Jul;9(7):1945-55. DOI:
10.1158/1535-7163.MCT-10-0053[2] Cheon JH, et al. The JAK2 inhibitors CEP-33779 and NVP-BSK805 have high P-gp inhibitory activity and sensitize drug-resistant cancer cells to vincristine. Biochem Biophys Res Commun. 2017 Sep 2;490(4):1176-1182. DOI:
10.1016/j.bbrc.2017.06.178
